This invention relates to amino acid-containing therapeutic compounds.
Luteinizing hormone (LH) and follicle-stimulating hormone (FSH) are gonadotropic hormones produced by the pituitary gland of humans and animals. LH and FSH are released from the pituitary gland by the action of LH- and FSH-releasing hormone (LHRH). Naturally-occuring LHRH has been shown to be a decapeptide of the formula (pyro)-Glu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH.sub.2 ; A. V. Schally et al., Biochem. Biophys. Res. Comm., 43, 393 and 1334 (1971). (Herein, where no isomeric designation is given, the naturally occurring L-form is meant.)
A large number of patents and publications described LHRH analogs and their use in various medical applications. For example, Schally and Coy U.S. Pat. No. 4,010,125 describes a decapeptide analogue of LHRH of the formula (pyro)-Glu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH.sub.2 useful for inducing ovulation and for treating delayed puberty and hypogonadism.
Tolis et al. Proc. Natl. Acad. Sci. 79, 1658-1662 (1982) suggests that the chronic administration of large doses of two LHRH analogues ([D-Trp.sup.6 ] LHRH and [D-Ser(But).sup.6 ]des-Gly-NH.sub.2.sup.10 -LHRH) can result in the suppression of pituitary and leydig cell production and the regression of mammary and prostatic endocrine-dependent tumors in animals and humans.
Johnson et al. U.S. Pat. No. 4,071,622 describes nonapeptides of the formula pGlu-His-Trp-Ser-Tyr-X-Leu-Arg-Pro-NH-C.sub.2 H.sub.5, where X is the D form of Tyr, Trp, or Phe, useful for the treatment of mammary tumors.